Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors-Reference-Cited by-同舟云学术

Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors

Published:2019-10-22 Issue:11 Volume:10 Page:1549-1553
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

De Clercq Dries J. H.¹²,Heppner David E.¹²^ORCID,To Ciric³⁴⁵,Jang Jaebong¹²,Park Eunyoung¹²,Yun Cai-Hong¹²⁶^ORCID,Mushajiang Mierzhati³,Shin Bo Hee³,Gero Thomas W.¹²,Scott David A.¹²,Jänne Pasi A.³⁴⁵⁷,Eck Michael J.¹²,Gray Nathanael S.¹²^ORCID

Affiliation:

1. Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States

2. Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States

3. Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States

4. Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States

5. Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215, United States

6. Department of Biochemistry and Biophysics, Peking University Health Science Center, Beijing 100191, China

7. Belfer Center for Applied Cancer Science, Boston, Massachusetts 02215, United States

Funder

National Cancer Institute

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.9b00381

Reference22 articles.

1. EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

2. Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

3. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

4. EGFRMutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib

5. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

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